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4,5-dihydrothiazole carboxylic acid derivative containing sulfonylhydrazine structure, and preparation method and application thereof

A dihydrothiazole carboxylic acid and sulfonyl hydrazide-containing technology, which is applied in 4 fields, can solve problems such as few research reports, and achieve the effect of broad application prospects

Pending Publication Date: 2020-02-07
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most natural products cannot fully meet the requirements of being used as pesticides, and structural modification and optimization are required
4,5-Dihydrothiazole carboxylic acid compounds are a class of natural products with various biological activities such as antitumor, antibacterial and antiviral, and have received extensive attention and research in the medical field. rarely reported

Method used

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  • 4,5-dihydrothiazole carboxylic acid derivative containing sulfonylhydrazine structure, and preparation method and application thereof
  • 4,5-dihydrothiazole carboxylic acid derivative containing sulfonylhydrazine structure, and preparation method and application thereof
  • 4,5-dihydrothiazole carboxylic acid derivative containing sulfonylhydrazine structure, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Synthesis of (R)-N'-(2-phenyl-4,5-dihydrothiazole-4-carbonyl)benzenesulfonylhydrazide (derivative 01)

[0026] 1) Step: Preparation of (R)-N'-(2-phenyl-4,5-dihydrothiazole-4-carbonyl)benzenesulfonylhydrazide

[0027] In a three-neck round bottom flask, add 20.0 mL of dry dichloromethane, add (R)-2-phenyl-4,5-dihydrothiazole-4-carboxylic acid (1.0 mmol) to the above system, and reduce to 0 ℃, monitor the temperature with a thermometer, add N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (EDCI, 1.20mmol) and 1-hydroxybenzotriazole (HOBt , 1.06mmol), after the addition, the reaction system was slowly raised to room temperature after 0.5h, and stirred at room temperature. ) was slowly added to the above reaction system, after the addition was completed, it was slowly raised to room temperature, and the reaction was monitored by TLC. After the reaction was completed, 20.0 mL of dichloroethane was added to dilute, and then water, 1mol / L hydrochloric acid solutio...

Embodiment 2

[0035] Utilize derivatives (01~15) provided by the present invention to test, verify the biological activity evaluation to germ:

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Abstract

The invention relates to a 4,5-dihydrothiazole carboxylic acid derivative which is represented by a general formula (I) and has a sulfonylhydrazine structure and bactericidal activity, and a preparation method and application thereof. (R)-2-aryl-4,5-dihydrothiazole-4-carboxylic acid of different substituted natural source compounds and phenylsulfonyl hydrazide, wherein (R)-2-aryl-4,5-dihydrothiazole-4-carboxylic acid of different substituted natural source compounds is spliced with phenyl sulfonylhydrazine, wherein R1-R10 are defined in the specification. The technical effects are as the follows that the 4,5-dihydrothiazole carboxylic acid derivative which has broad-spectrum bactericidal activity and contains the sulfonylhydrazine structure is found, and the 4,5-dihydrothiazole carboxylicacid derivative is an ecological bactericide with a wide application prospect.

Description

technical field [0001] The invention relates to the synthesis technology of agricultural fungicides based on natural sources, in particular to a class of 4,5-dihydrothiazole carboxylic acid derivatives containing a sulfonyl hydrazide structure and a preparation method and application thereof. Background technique [0002] Natural products are a huge treasure trove of resources, and finding pesticide active compounds from the treasure trove of natural resources has become an important approach and research hotspot for the creation of new pesticides. However, most natural products cannot fully meet the requirements as pesticides and need to be modified and optimized. 4,5-Dihydrothiazole carboxylic acid compounds are a class of natural products with various biological activities such as antitumor, antibacterial and antiviral, and have received extensive attention and research in the medical field. Rarely reported. Compared with traditional chemically synthesized pesticides, n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/12A01N51/00A01P3/00
CPCC07D277/12A01N51/00
Inventor 李凤云李根龚珈苧李鑫韩永艳
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE